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PNU 177864 hydrochloride

Highly selective D3 antagonist CAS# 250266-51-4

PNU 177864 hydrochloride

Catalog No. BCC7664----Order now to get a substantial discount!

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PNU 177864 hydrochloride: 5mg $92 In Stock
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Chemical structure

PNU 177864 hydrochloride

3D structure

Chemical Properties of PNU 177864 hydrochloride

Cas No. 250266-51-4 SDF Download SDF
PubChem ID 9887351 Appearance Powder
Formula C18H21F3N2O3S M.Wt 402.4
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 20 mM in water and to 100 mM in DMSO
Chemical Name N-[4-[2-(propylamino)ethyl]phenyl]-4-(trifluoromethoxy)benzenesulfonamide
SMILES CCCNCCC1=CC=C(C=C1)NS(=O)(=O)C2=CC=C(C=C2)OC(F)(F)F
Standard InChIKey JGGQWSXZZQPZTR-UHFFFAOYSA-N
Standard InChI InChI=1S/C18H21F3N2O3S/c1-2-12-22-13-11-14-3-5-15(6-4-14)23-27(24,25)17-9-7-16(8-10-17)26-18(19,20)21/h3-10,22-23H,2,11-13H2,1H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PNU 177864 hydrochloride

DescriptionHighly selective dopamine D3 receptor antagonist. Induces phospholipidosis and exhibits antischizophrenic activity in vivo.

PNU 177864 hydrochloride Dilution Calculator

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PNU 177864 hydrochloride Molarity Calculator

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Preparing Stock Solutions of PNU 177864 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4851 mL 12.4254 mL 24.8509 mL 49.7018 mL 62.1272 mL
5 mM 0.497 mL 2.4851 mL 4.9702 mL 9.9404 mL 12.4254 mL
10 mM 0.2485 mL 1.2425 mL 2.4851 mL 4.9702 mL 6.2127 mL
50 mM 0.0497 mL 0.2485 mL 0.497 mL 0.994 mL 1.2425 mL
100 mM 0.0249 mL 0.1243 mL 0.2485 mL 0.497 mL 0.6213 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on PNU 177864 hydrochloride

Myopathy related to administration of a cationic amphiphilic drug and the use of multidose drug distribution analysis to predict its occurrence.[Pubmed:15204973]

Toxicol Pathol. 2004 May-Jun;32(3):318-25.

Many cationic amphiphilic (phospholipidosis-inducing) drugs (CADs) accumulate in tissues following repeated dosing in preclinical models, and this is sometimes associated with dose-limiting toxicities. Plasma drug levels cannot be used to estimate tissue accumulation of CADs since it occurs in tissues despite stabilization of plasma levels. Severe myopathy was found in skeletal muscles of rats during the initial safety evaluation of a dopamine D3 receptor antagonist, PNU-177864, and was associated with phospholipidosis in numerous tissues. The myopathy was observed only when plasma levels of PNU-177864 remained essentially constant throughout the 24-hour dosing period. A repeat dose drug distribution study using whole body autoradiography demonstrated that drug-related material did not accumulate in skeletal muscle or other tissues following repeated doses at levels considered within the therapeutic range and showing toxicokinetic profiles acceptable for further development. These observations provided support for the continued development of and longer-term toxicity studies with this candidate compound.

Epididymal and systemic phospholipidosis in rats and dogs treated with the dopamine D3 selective antagonist PNU-177864.[Pubmed:15204974]

Toxicol Pathol. 2004 May-Jun;32(3):326-32.

Repeat dose oral toxicity studies were conducted in rat and dog to assess the safety for human clinical testing of the potent dopamine D3 receptor antagonist, PNU-177864. Systemic phospholipidosis was the principal treatment-related change with epididymal epithelial cell phospholipidosis being the most prominent finding in rats and dogs. Epididymal epithelial cells had no histologic evidence of degeneration; sperm density and morphology were normal histologically in both species; and sperm concentration, morphology, and motility in the dog were comparable to dogs given vehicle. Other sites with phospholipidosis included lymphoid tissues (lymph nodes, Peyer's patches, and/or spleen), pulmonary alveolar macrophages, and peripheral blood lymphocytes in rats and dogs and adrenal cortex, liver, pituitary, hair follicles, bone marrow lymphocytes and plasma cells, and skeletal muscle in rats only. The phospholipidosis was resolved after a 6-week recovery period in all tissues but epididymis. There was no evidence of cell injury in tissues that had phospholipid accumulations except in rat skeletal muscle that had multifocal myofiber degeneration and necrosis. For clinical trials, serum AST and CK and peripheral blood lymphocyte vacuolation were considered potential safety biomarkers for skeletal muscle degeneration and phospholipidosis, respectively.

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